Dimethyl Sulfoxide
Apexbio Technology LLC THZ2 1604810-84-5 10mM (in 1mL DMSO)
THZ2 (CAS 1604810-84-5) is a selective inhibitor of cyclin-dependent kinase 7 (CDK7) demonstrating an IC50 of 13 9 nM CDK7 a serine/threonine kinase bound and activated by cyclins regulates cell cycle progression and transcriptional control through phosphorylation of RNA polymerase II (RNAPII) In triple-negative breast cancer (TNBC) cell models THZ2 reduces cellular proliferation induces apoptotic cell death without affecting cell-cycle distribution and inhibits colony formation at low-nanomolar concentrations (IC50 10 nM) In xenograft mouse models THZ2 suppresses tumor growth without noticeable toxicity Thus THZ2 is useful in research investigating CDK7-mediated oncogenic mechanisms in cancer
Apexbio Technology LLC Bexarotene 153559-49-0 10mM (in 1mL DMSO)
Bexarotene is a synthetic selective agonist for retinoid X receptors (RXRs) a subclass of nuclear hormone receptors involved in the regulation of gene transcription Upon binding to RXRs Bexarotene modulates the expression of target genes associated with cell differentiation proliferation and apoptosis Due to this mechanism Bexarotene is commonly employed in research investigating tumor growth inhibition cellular differentiation pathways and apoptosis induction Researchers also frequently utilize this retinoid derivative to elucidate RXR-mediated signaling pathways in oncology and to explore potential therapeutic applications for various malignancies
Apexbio Technology LLC Simvastatin (Zocor) 79902-63-9 10mM (in 1mL DMSO)
Simvastatin (CAS 79902-63-9) marketed as Zocor is a synthetic lactone derived from fermented Aspergillus terreus metabolites Following oral administration the inactive lactone is hydrolyzed into an active -hydroxy acid metabolite which specifically inhibits HMG-CoA reductase the rate-limiting enzyme in cholesterol biosynthesis Simvastatin demonstrates antiproliferative effects in hepatocellular carcinoma cells (HepG2 Huh7) inducing apoptosis cell cycle arrest at G0/G1 reducing expression of cyclins (D1 E) and cyclin-dependent kinases (CDK1 2 4) while elevating CDK inhibitors p19 and p27 It is therefore utilized extensively for research in cancer biology cardiovascular pathology and lipid metabolism disorders
Apexbio Technology LLC Cyclo (-RGDfK) 161552-03-0 10mM (in 1mL DMSO)
Cyclo(-RGDfK) is a cyclic pentapeptide that functions as an inhibitor targeting the integrin v 3 Integrins are transmembrane receptors mediating cell adhesion by recognizing specific peptide sequences notably the Arg-Gly-Asp (RGD) motif Integrin v 3 is involved in cell adhesion processes such as angiogenesis tissue remodeling and tumor development and is abundantly expressed on activated endothelial cells and various tumor cells Cyclo(-RGDfK) specifically binds integrin v 3 disrupting integrin-mediated cell attachment Consequently it is frequently utilized in bioengineering applications to modify biomaterial surfaces for enhanced cellular adherence and integration Additionally cyclo(-RGDfK) serves as a targeting ligand in imaging probes aimed at localizing integrin-positive tissues in cancer research
Apexbio Technology LLC INK 128 (MLN0128) 1224844-38-5 10mM (in 1mL DMSO)
INK 128 (MLN0128 CAS 1224844-38-5) is a selective inhibitor of the mammalian target of rapamycin (mTOR) a conserved serine/threonine kinase integral to the PI3K/AKT/mTOR signaling pathway This compound inhibits both mTOR complexes (mTORC1 and mTORC2) demonstrating an IC50 of approximately 1 nM In preclinical studies utilizing human pancreatic and HER2-positive breast cancer cell lines INK 128 significantly reduced cellular proliferation and viability via concentration- and time-dependent suppression of mTOR activity Moreover it exhibited notable tumor suppression in breast cancer xenograft models enhancing efficacy when combined with agents such as sorafenib sunitinib paclitaxel or lapatinib highlighting its potential value for oncology research and therapeutic development
Apexbio Technology LLC Etodolac 41340-25-4 10mM (in 1mL DMSO)
Etodolac (CAS 41340-25-4) is a selective cyclooxygenase-2 (COX-2) inhibitor belonging to the class of non-steroidal anti-inflammatory drugs (NSAIDs) It exhibits inhibitory activity against COX-2 with an IC50 of 53 5 nM Etodolac is commonly utilized for research involving inflammatory conditions such as osteoarthritis and rheumatoid arthritis In isolated rabbit articular chondrocytes stimulated with TNF Etodolac prevented apoptotic cell shrinkage and suppressed caspase-3/7 activation Conversely in human malignant rhabdoid tumor cells (FRTK-1) Etodolac induced apoptosis in a dose-dependent manner increasing activities of caspase-3 -8 and -9
Apexbio Technology LLC DMOG 89464-63-1 10mM (in 1mL DMSO)
DMOG (Dimethyloxalylglycine CAS 89464-63-1) is a small molecule inhibitor of prolyl-4-hydroxylase domain (PHD) enzymes thereby modulating the stability of hypoxia-inducible factor (HIF) PHD inhibition by DMOG prevents HIF-1 prolyl hydroxylation and subsequent degradation stabilizing HIF-1 protein even under normoxic conditions (0 1 1 mmol/L in vitro) Additionally DMOG treatment suppresses NF- B signaling during LPS-induced inflammatory responses in animal models improving survival rates and enhancing IL-10 expression predominantly in peritoneal B-1 cells Thus DMOG serves as a valuable research tool to explore hypoxia signaling pathways and inflammatory responses
Apexbio Technology LLC Wortmannin 19545-26-7 10mM (in 1mL DMSO)
Wortmannin is a selective inhibitor targeting phosphatidylinositol-3-kinase (PI3K) with reported IC50 of approximately 1 9 nM It inhibits PI3K through an ATP-noncompetitive binding mechanism interacting directly with the catalytic region Additionally wortmannin functions as a noncompetitive inhibitor of myosin light chain kinase (MLCK) with an IC50 around 1 9 M thus decreasing myosin light chain phosphorylation and associated smooth muscle contraction In biomedical research wortmannin is commonly employed to dissect the PI3K signaling pathway evaluate smooth muscle contractility and explore therapeutic potentials related to vascular dilation and inflammation modulation
Apexbio Technology LLC TAE226 (NVP-TAE226) 761437-28-9 10mM (in 1mL DMSO)
TAE226 (NVP-TAE226 CAS 761437-28-9) is a selective inhibitor targeting focal adhesion kinase (FAK) with an IC50 of 5 5 nM and it also inhibits the related protein tyrosine kinase Pyk2 (IC50 3 5 nM) By suppressing FAK activity crucial for cell adhesion and migration TAE226 influences cellular processes associated with tumor progression Studies using glioma cells (including U87 and variants) and medullary thyroid carcinoma line MZ-CRC-1 revealed that TAE226 decreases cell proliferation invasion and induces apoptosis highlighting its potential value in cancer research
Apexbio Technology LLC PD318088 391210-00-7 10mM (in 1mL DMSO)
PD318088 (CAS 391210-00-7) is an allosteric non-ATP competitive inhibitor of MEK1/2 kinase activity Structurally related to PD184352 it interacts adjacent to the ATP-binding site of MEK1 in proximity to residues Ile216 Phe209 Arg189 and Asp190 stabilizing a ternary complex involving MEK1/2 and MgATP This binding moderately increases the dissociation constant (Kd) for the MEK dimerization state from 75 nM to 140 nM PD318088 is mainly utilized as a molecular tool in protein kinase signaling research particularly in pathways involving MEK1/2
Apexbio Technology LLC Sulfamethazine 57-68-1 10mM (in 1mL DMSO)
Sulfamethazine (Sulfadimidine) is a sulfonamide antimicrobial agent that exerts antibacterial activity by competitively inhibiting bacterial dihydropteroate synthase an enzyme crucial for the synthesis of folic acid in bacteria Through this enzyme inhibition sulfamethazine disrupts bacterial folate metabolism impairing bacterial DNA and protein synthesis pathways In biomedical research this compound is commonly employed as an investigative tool for studying bacterial infections particularly in animal models representing respiratory and gastrointestinal infections attributed to susceptible bacterial strains In vitro studies report IC50 values for bacterial dihydropteroate synthase inhibition typically ranging from 5 to 50 M depending on experimental conditions and bacterial species tested Additionally sulfamethazine serves as a reference compound in research examining antimicrobial resistance and pharmacokinetic parameters
Apexbio Technology LLC Methotrexate 59-05-2 10mM (in 1mL DMSO)
Methotrexate is a folate antagonist commonly utilized in biomedical research due to its inhibitory action on dihydrofolate reductase (DHFR) a critical enzyme in folate metabolism This inhibition disrupts nucleotide synthesis thereby interfering with cell proliferation Upon cell uptake methotrexate is converted intracellularly into polyglutamate derivatives which prolong its biochemical activity through sustained enzyme inhibition Additionally methotrexate promotes extracellular adenosine release at inflammatory sites mediating immunological effects In cellular assays for DHFR inhibition methotrexate demonstrates potent inhibitory activity with reported IC50 values typically ranging from 5 to 50 nM depending on the cell type and experimental conditions Methotrexate is widely utilized in research on inflammation oncology and rheumatoid arthritis-related mechanisms
Apexbio Technology LLC Hesperadin 422513-13-1 10mM (in 1mL DMSO)
Hesperadin is a small-molecule ATP-competitive inhibitor targeting Aurora B kinase a serine/threonine-protein kinase involved in mitotic regulation By occupying the ATP-binding pocket of Aurora B and adjacent hydrophobic regions Hesperadin suppresses kinase activity with an IC50 approximately 250 nM In mitotic cells Aurora B-mediated phosphorylation of histone H3 Ser-10 is inhibited by Hesperadin this phosphorylation event is widely utilized as a mitotic biomarker Furthermore experimental applications of Hesperadin include investigating cell-cycle dynamics chromosome alignment and spindle checkpoint mechanisms as evidenced by its ability to disrupt proper chromosome alignment and segregation at approximately 40 nM IC50
Apexbio Technology LLC Tie2 kinase inhibitor 948557-43-5 10mM (in 1mL DMSO)
Tie2 kinase inhibitor (CAS 948557-43-5) is a selective and reversible small-molecule inhibitor targeting the Tie2 receptor tyrosine kinase a critical modulator of endothelial cell survival angiogenesis and vascular integrity By inhibiting Tie2 autophosphorylation this compound disrupts subsequent signaling pathways involved in endothelial maturation and tumor-associated angiogenesis In vitro studies demonstrate potent inhibition of Tie2 kinase activity (IC50 0 25 M) with substantial selectivity over other kinases including p38 In vivo treatment reduces angiogenesis and tumor progression in murine xenograft tumor models This inhibitor is thus relevant for research examining angiogenic mechanisms and cancer progression
Apexbio Technology LLC Pranlukast 103177-37-3 10mM (in 1mL DMSO)
Pranlukast (CAS 103177-37-3) is a selective antagonist of cysteinyl leukotriene (cysLT) receptors exhibiting its pharmacological action by competitively binding to targeted leukotriene receptor sites It specifically prevents the interaction of endogenous leukotrienes (LTC4 LTD4 LTE4) with corresponding receptors located on pulmonary cell membranes thus reducing leukotriene-driven airway inflammation and bronchoconstriction Binding experiments demonstrate that pranlukast possesses notably greater affinity for LTE4 and LTD4 compared to LTC4 In biomedical research pranlukast is frequently utilized for mechanistic studies and pharmacological modeling of asthma allergic rhinitis and related airway inflammatory conditions